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. Author manuscript; available in PMC: 2016 Mar 1.
Published in final edited form as: Bioorg Med Chem. 2015 Jan 13;23(5):1027–1043. doi: 10.1016/j.bmc.2015.01.011

Table 1.

Activity and cytotoxicity of T3SS inhibitors with varying substituents at the α-position.

graphic file with name nihms660087t1.jpg
Compound
#		 R R’ secretion
IC50 (µM)		 translocation
IC50 (µM)		 translocation
CC50 (µM)
1 −Me −H 7.8 ± 2.0 11 ± 2 >100
6a −H −H >100 n.d. n.d.
6b −Me −Me >100 n.d. n.d.
6c −Et −H 3.9 ± 1.3 3.0 ± 1.0 67 ± 18
6d −nPr −H >100 n.d. n.d.
6e −iPr −H >100 n.d. n.d.
(R)-1 −Me (R) −H 4.3 ± 1.5 8.9 ± 5.5 61 ± 19
(S)-1 −Me (S) −H >100 n.d. n.d.

n.d.: value not determined